About: Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor     Goto   Sponge   NotDistinct   Permalink

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Description
  • yclin-dependent kinases (CDK) are key pos. regulators of cell cycle progression and attractive targets in oncol. SCH 727965 inhibits CDK2, CDK5, CDK1, and CDK9 activity in vitro with IC50 values of 1, 1, 3, and 4 nmol/L, resp. SCH 727965 was selected as a clin. candidate using a functional screen in vivo that integrated both efficacy and safety parameters. Compared with flavopiridol, SCH 727965 exhibits superior activity with an improved therapeutic index. In cell-based assays, SCH 727965 completely suppressed retinoblastoma phosphorylation, which correlated with apoptosis onset and total inhibition of bromodeoxyuridine incorporation in >100 tumor cell lines of diverse origin and background. Moreover, short exposures to SCH 727965 were sufficient for long-lasting cellular effects. SCH 727965 induced regression of established solid tumors in a range of mouse models following intermittent scheduling of doses below the maximally tolerated level. This was assocd.
  • yclin-dependent kinases (CDK) are key pos. regulators of cell cycle progression and attractive targets in oncol. SCH 727965 inhibits CDK2, CDK5, CDK1, and CDK9 activity in vitro with IC50 values of 1, 1, 3, and 4 nmol/L, resp. SCH 727965 was selected as a clin. candidate using a functional screen in vivo that integrated both efficacy and safety parameters. Compared with flavopiridol, SCH 727965 exhibits superior activity with an improved therapeutic index. In cell-based assays, SCH 727965 completely suppressed retinoblastoma phosphorylation, which correlated with apoptosis onset and total inhibition of bromodeoxyuridine incorporation in >100 tumor cell lines of diverse origin and background. Moreover, short exposures to SCH 727965 were sufficient for long-lasting cellular effects. SCH 727965 induced regression of established solid tumors in a range of mouse models following intermittent scheduling of doses below the maximally tolerated level. This was assocd. (en)
Title
  • Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor
  • Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor (en)
skos:prefLabel
  • Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor
  • Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor (en)
skos:notation
  • RIV/00216224:14310/10:00045047!RIV11-MSM-14310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • N
http://linked.open...iv/cisloPeriodika
  • 8
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 254508
http://linked.open...ai/riv/idVysledku
  • RIV/00216224:14310/10:00045047
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • kinase; cdk; inhibitor; cancer (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [9F0357DB5342]
http://linked.open...i/riv/nazevZdroje
  • Molecular Cancer Therapeutics
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 2010
http://linked.open...iv/tvurceVysledku
  • Davis, Nicole
  • Dwyer, Michael
  • Fischmann, Thierry
  • Guzi, Timothy
  • Parry, David
  • Paruch, Kamil
  • Seghezzi, Wolfgang
  • Wiswell, Derek
  • Shanahan, Frances
  • Chen, ´Taiying
  • Doll, Ronald
  • Kirschmeier, Paul
  • Lees, Emma
  • Nomeir, Amin
  • Oft, Martin
  • Prabhavalkar, Deepa
  • Wang, Yaolin
  • Windsor, William
issn
  • 1535-7163
number of pages
http://localhost/t...ganizacniJednotka
  • 14310
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